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Assay Detail

CHEMBL4386711

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of NS5A in HCV genotype 2a JFH1 infected in human HuH7 replicon cells assessed as reduction in viral replication after 3 days by luciferase reporter gene assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Hepatitis C virus subtype 2a
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Nonstructural protein 5A (CHEMBL3307224)
Type SINGLE PROTEIN
Organism Hepatitis C virus

Publication

Discovery of velpatasvir (GS-5816): A potent pan-genotypic HCV NS5A inhibitor in the single-tablet regimens Vosevi<sup>®</sup> and Epclusa<sup>®</sup>.
Link JO, Taylor JG, Trejo-Martin A, Kato D, Katana AA, Krygowski ES, Yang ZY, Zipfel S, Cottell JJ, Bacon EM, Tran CV, Yang CY, Wang Y, Wang KW, Zhao G, Cheng G, Tian Y, Gong R, Lee YJ, Yu M, Gorman E, Mogalian E, Perry JK.
Bioorg Med Chem Lett (2019) 29 : 2415 -2427
PubMed 31230974 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 9.21 10.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4473265 1 10.74
CHEMBL2374220 LEDIPASVIR 4.0 1 7.68
CHEMBL3545062 VELPATASVIR 4.0 1 -
CHEMBL4516340 1 -
CHEMBL4468617 1 -
CHEMBL4457264 1 -
CHEMBL4574152 1 -
CHEMBL4467926 1 -
CHEMBL4557789 1 -
CHEMBL4587426 1 -
CHEMBL4547877 1 -
CHEMBL4437858 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4473265 EC50 = 0.018 nM 10.74
CHEMBL2374220 LEDIPASVIR EC50 = 21.0 nM 7.68
CHEMBL3545062 VELPATASVIR EC50 = 0.008 nM -
CHEMBL4516340 EC50 = 0.004 nM -
CHEMBL4468617 EC50 = 0.006 nM -
CHEMBL4457264 EC50 = 0.008 nM -
CHEMBL4574152 EC50 = 0.005 nM -
CHEMBL4467926 EC50 = 0.006 nM -
CHEMBL4557789 EC50 = 0.006 nM -
CHEMBL4587426 EC50 = 0.006 nM -
CHEMBL4547877 EC50 = 0.007 nM -
CHEMBL4437858 EC50 = 0.004 nM -